EA201690818A1 - SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR APPLICATION AS SYK INHIBITORS - Google Patents

SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR APPLICATION AS SYK INHIBITORS

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Publication number
EA201690818A1
EA201690818A1 EA201690818A EA201690818A EA201690818A1 EA 201690818 A1 EA201690818 A1 EA 201690818A1 EA 201690818 A EA201690818 A EA 201690818A EA 201690818 A EA201690818 A EA 201690818A EA 201690818 A1 EA201690818 A1 EA 201690818A1
Authority
EA
Eurasian Patent Office
Prior art keywords
application
pyrimidine compounds
substituted pyrimidine
syk inhibitors
formula
Prior art date
Application number
EA201690818A
Other languages
Russian (ru)
Other versions
EA030962B1 (en
Inventor
Джекиу Ли
Джанг-сик Чой
Хае-Джун Хванг
Хо-Джун Сонг
Джунг-хо Ким
Се-Вон Ким
Джонг Сунг Кох
Джаесанг Ли
Тае-Им Ли
Юнг-геун Чой
Сунг-Хо Парк
Ин Йонг Ли
Бьюнг-Чул Сух
Пареш Девидас Салгаонкар
Донг-Сик Джунг
Original Assignee
Джиноско
Оскотек, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Джиноско, Оскотек, Инк. filed Critical Джиноско
Publication of EA201690818A1 publication Critical patent/EA201690818A1/en
Publication of EA030962B1 publication Critical patent/EA030962B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Otolaryngology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Раскрываются соединения формулы (I) и способы ингибирования киназ, включая тирозинкиназы селезенки. Также раскрываются способы лечения опосредованного киназами заболевания или состояния посредством введения субъекту терапевтически эффективного количества соединения формулы (I).Compounds of formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to the subject a therapeutically effective amount of a compound of formula (I).

EA201690818A 2013-10-21 2014-10-21 Substituted pyrimidine compounds and their use as syk inhibitors EA030962B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361893866P 2013-10-21 2013-10-21
PCT/US2014/061649 WO2015061369A1 (en) 2013-10-21 2014-10-21 Substituted pyrimidine compounds and their use as syk inhibitors

Publications (2)

Publication Number Publication Date
EA201690818A1 true EA201690818A1 (en) 2016-08-31
EA030962B1 EA030962B1 (en) 2018-10-31

Family

ID=52826699

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690818A EA030962B1 (en) 2013-10-21 2014-10-21 Substituted pyrimidine compounds and their use as syk inhibitors

Country Status (22)

Country Link
US (1) US9212178B2 (en)
EP (1) EP3060562B1 (en)
JP (1) JP6434506B2 (en)
KR (1) KR102228034B1 (en)
CN (1) CN105940000B (en)
AU (1) AU2014340249B2 (en)
BR (1) BR112016008060A8 (en)
CL (1) CL2016000939A1 (en)
EA (1) EA030962B1 (en)
ES (1) ES2890552T3 (en)
HK (1) HK1226395A1 (en)
HU (1) HUE056048T2 (en)
IL (1) IL244817B (en)
MX (1) MX2016004841A (en)
MY (1) MY184561A (en)
NZ (1) NZ718576A (en)
PH (1) PH12016500735A1 (en)
PL (1) PL3060562T3 (en)
PT (1) PT3060562T (en)
SA (1) SA516370989B1 (en)
SG (1) SG11201602566XA (en)
WO (1) WO2015061369A1 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113248472B (en) * 2020-02-12 2022-06-28 中国药科大学 Anti-osteoporosis compound and derivative thereof, pharmaceutical composition, preparation method and application
KR20210152312A (en) * 2020-06-08 2021-12-15 주식회사 종근당 4-(4,5-dihydro-1h-pyrazol-1-yl)pyrimidine compound as cannabinoid receptor (cb1 receptor) antagonists and pharmaceutical composition including the same

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
AU2003301433A1 (en) 2002-10-16 2004-05-04 Millennium Pharmaceuticals, Inc. Spleen tyrosine kinase catalytic domain:crystal structure and binding pockets thereof
SE0300119D0 (en) * 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
SE0300120D0 (en) * 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
NZ541218A (en) * 2003-01-17 2008-05-30 Astrazeneca Ab Thienopyrimidinediones and their use in modulation of autoimmune disease
EA200800664A1 (en) * 2005-10-13 2009-02-27 Глаксо Груп Лимитед PYRROPOLYMIDINE DERIVATIVES AS SYK INHIBITORS
AU2008296479A1 (en) * 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
WO2010015520A1 (en) 2008-08-05 2010-02-11 Boehringer Ingelheim International Gmbh Substituted naphthyridines and use thereof as medicines
WO2010015518A2 (en) 2008-08-05 2010-02-11 Boehringer Ingelheim Interntional Gmbh 4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments
EA024729B1 (en) * 2009-11-13 2016-10-31 Джиноско Kinase inhibitors
WO2011092128A1 (en) 2010-01-29 2011-08-04 Boehringer Ingelheim International Gmbh Substituted naphthyridines and their use as syk kinase inhibitors
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
CN103003281A (en) 2010-05-20 2013-03-27 弗·哈夫曼-拉罗切有限公司 Pyrrolo [2, 3 - b] pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
WO2011156698A2 (en) * 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
UY34484A (en) * 2011-12-15 2013-07-31 Bayer Ip Gmbh BENZOTIENILO-PIRROLOTRIAZINAS DISUSTITUIDAS AND ITS USES
EP2804861B1 (en) * 2012-01-20 2018-02-28 Genosco Substituted pyrimidine compounds and their use as syk inhibitors
EA031267B1 (en) * 2012-03-22 2018-12-28 Оскотек, Инк. Substituted pyridopyrimidine compounds and their use as flt3 inhibitors

Also Published As

Publication number Publication date
JP6434506B2 (en) 2018-12-05
PL3060562T3 (en) 2022-01-10
EP3060562A4 (en) 2017-06-14
CN105940000B (en) 2019-12-24
PH12016500735A1 (en) 2016-05-30
EP3060562A1 (en) 2016-08-31
MY184561A (en) 2021-04-03
WO2015061369A1 (en) 2015-04-30
PT3060562T (en) 2021-09-02
US20150111883A1 (en) 2015-04-23
SG11201602566XA (en) 2016-05-30
AU2014340249A1 (en) 2016-04-28
HUE056048T2 (en) 2022-01-28
SA516370989B1 (en) 2018-04-05
BR112016008060A8 (en) 2020-03-17
CN105940000A (en) 2016-09-14
JP2016534054A (en) 2016-11-04
EP3060562B1 (en) 2021-07-28
CL2016000939A1 (en) 2016-11-11
ES2890552T3 (en) 2022-01-20
EA030962B1 (en) 2018-10-31
AU2014340249B2 (en) 2017-05-25
HK1226395A1 (en) 2017-09-29
NZ718576A (en) 2019-11-29
US9212178B2 (en) 2015-12-15
KR102228034B1 (en) 2021-03-16
MX2016004841A (en) 2016-07-26
IL244817B (en) 2019-07-31
KR20160068967A (en) 2016-06-15
IL244817A0 (en) 2016-05-31

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